Synthesis and biological evaluation of quinoxaline di-N-oxide derivatives with in vitro trypanocidal activity

被引：18
|
作者：
Perez-Silanes, Silvia [1 ,2 ]
Torres, Enrique [1 ]
Arbillaga, Leire [3 ]
Varela, Javier [4 ]
Cerecetto, Hugo [4 ]
Gonzalez, Mercedes [4 ]
Azqueta, Amaya [3 ,5 ]
Moreno-Viguri, Elsa [1 ,2 ]
机构：
[1] Univ Navarra, Dept Organ & Pharmaceut Chem, Irunlarrea S-N, Pamplona 31008, Spain
[2] Univ Navarra, Inst Trop Hlth, Irunlarrea S-N, Pamplona 31008, Spain
[3] Univ Navarra, Dept Pharmacol & Toxicol, Irunlarrea S-N, Pamplona 31008, Spain
[4] Univ Republica, Fac Ciencias, Lab Quim Organ, Grp Quim Med, Igua 4225, Montevideo 11400, Uruguay
[5] Recinto Complejo Hosp Navarra, Navarra Inst Hlth Res, IdiSNA, C Irunlarrea 3, Pamplona 31008, Spain
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 03期
关键词：
Chagas disease; Trypanosoma cruzi; Quinoxaline N-oxide; Cytotoxicity; Genotoxicity; 1,4-DI-N-OXIDE DERIVATIVES; CHAGAS-DISEASE; N-1; N-4-DIOXIDE DERIVATIVES; ANTITRYPANOSOMAL ACTIVITY; ANTIBACTERIAL ACTIVITY; ANTICHAGASIC AGENTS; FLUOROQUINOLONES; IDENTIFICATION; SUBSTITUTIONS; TUBERCULOSIS;
D O I：
10.1016/j.bmcl.2015.12.070
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We report the synthesis and in vitro activity against Trypanosoma cruzi epimastigotes of 15 novel quinoxaline derivatives. Ten of the derivatives presented IC50 values lower than the reference drugs Nfx and Bzn; four of them standed out with IC50 values lower than 1.5 mu M. Moreover, unspecific cytotoxicity and genotoxicity studies are also reported. Compound 14 showed a SI higher than 24, whereas compound 10 was the only one that was negative in the genotoxicity screening. (C) 2015 Elsevier Ltd. All rights reserved.
引用
收藏
页码：903 / 906
页数：4
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